Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors

…, CE Roth, S Skala, G Jin, R Cowling, KM Mohler…

Index: Zask; Gu; Albright; Du; Hogan; Levin; Chen; Killar; Sung; DiJoseph; Sharr; Roth; Skala; Jin; Cowling; Mohler; Barone; Black; March; Skotnicki Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 8 p. 1487 - 1490

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Citation Number: 35

Abstract

Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.

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